Reuptake inhibitor: Difference between revisions

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A '''reuptake inhibitor''', also known as a transporter blocker, is a drug that inhibits the reuptake of a [[neurotransmitter]] from the synapse into the presynaptic neurone, leading to an increase in the extracellular concentrations of the neurotransmitter and therefore an increase in neurotransmission. Various drugs utilize reuptake inhibition to exert their psychological and physiological effects, including many antidepressants and ~~psychostimulants~~.

A '''reuptake inhibitor''', also known as a transporter blocker, is a drug that inhibits the reuptake of a [[neurotransmitter]] from the synapse into the presynaptic neurone, leading to an increase in the extracellular concentrations of the neurotransmitter and therefore an increase in neurotransmission. Various drugs utilize reuptake inhibition to exert their psychological and physiological effects, including many [[antidepressants]] and psycho[[stimulants]].

Most known reuptake inhibitors affect the monoamine neurotransmitters [[serotonin]], [[noradrenaline]] (and [[adrenaline]]), and [[dopamine]]. However there are also a number of pharmaceuticals and research chemicals that act as reuptake inhibitors for other neurotransmitters such as [[glutamate]], [[GABA]], glycine, adenosine, choline (the precursor of [[acetylcholine]]), and the endocannabinoids, among others.

Most known reuptake inhibitors affect the monoamine neurotransmitters [[serotonin]], [[noradrenaline]] (and [[adrenaline]]), and [[dopamine]]. However, there are also a number of pharmaceuticals and [[research chemicals]] that act as reuptake inhibitors for other neurotransmitters such as [[glutamate]], [[GABA]], glycine, adenosine, choline (the precursor of [[acetylcholine]]), and the endocannabinoids, among others.

==Mechanism of action==

[[File:Reuptake inhibitor.png|350px|thumb|right|The effect of reuptake inhibitors on the presynaptic neurone.]]

[[File:Reuptake inhibitor.png|350px|thumb|right|The effect of reuptake inhibitors on the presynaptic neurone]]

Standard reuptake inhibitors are believed to act simply as competitive substrates that work by binding directly to the plasmalemma transporter of the [[neurotransmitter]] in question. They occupy the transporter in place of the respective neurotransmitter and competitively block the neurotransmitter from being transported from the synapse into the presynaptic neurone.

Alternatively, some reuptake inhibitors bind to allosteric sites and inhibit reuptake indirectly and noncompetitively. Several dissociative drugs have been shown to work this way, including [[Phencyclidine|PCP]] and related drugs [[ketamine]], and dizocilpine (MK-801). They appear to exert their reuptake inhibition by binding to allosteric sites on each of the respective monoamine transporters. In addition to their high affinity for the main site of the monoamine transporters, several competitive transporter substrates, such as [[cocaine]], have lower affinity for these allosteric sites as well.

Alternatively, some reuptake inhibitors bind to allosteric sites and inhibit reuptake indirectly and noncompetitively. Several [[dissociative]] drugs have been shown to work this way, including [[Phencyclidine|PCP]] and related drugs [[ketamine]], and [[dizocilpine]] (MK-801). They appear to exert their reuptake inhibition by binding to allosteric sites on each of the respective monoamine transporters. In addition to their high affinity for the main site of the monoamine transporters, several competitive transporter substrates, such as [[cocaine]], have lower affinity for these allosteric sites as well.

==Types of reuptake inhibitors==

*A '''selective reuptake inhibitor''' will inhibit the reuptake of a specific [[neurotransmitter]]. An example of this is the class of antidepressants known as selective serotonin reuptake inhibitors, or SSRIs.

*A '''selective reuptake inhibitor''' will inhibit the reuptake of a specific [[neurotransmitter]]. An example of this is the class of antidepressants known as selective serotonin reuptake inhibitors, or [[SSRIs]].

*A '''non-selective reuptake inhibitor''' will inhibit the reuptake of more than one type of [[neurotransmitter]]. An example of this is [[cocaine]], which acts as a serotonin-noradrenaline-dopamine reuptake inhibitor, or SNDRI.

*A '''non-selective reuptake inhibitor''' will inhibit the reuptake of more than one type of [[neurotransmitter]]. An example of this is [[cocaine]], which acts as a serotonin-noradrenaline-dopamine reuptake inhibitor, or [[SNDRI]].

==See also==

@@ Line 1: / Line 1: @@
-A '''reuptake inhibitor''', also known as a transporter blocker, is a drug that inhibits the reuptake of a [[neurotransmitter]] from the synapse into the presynaptic neurone, leading to an increase in the extracellular concentrations of the neurotransmitter and therefore an increase in neurotransmission. Various drugs utilize reuptake inhibition to exert their psychological and physiological effects, including many antidepressants and psychostimulants.
+A '''reuptake inhibitor''', also known as a transporter blocker, is a drug that inhibits the reuptake of a [[neurotransmitter]] from the synapse into the presynaptic neurone, leading to an increase in the extracellular concentrations of the neurotransmitter and therefore an increase in neurotransmission. Various drugs utilize reuptake inhibition to exert their psychological and physiological effects, including many [[antidepressants]] and psycho[[stimulants]].
-Most known reuptake inhibitors affect the monoamine neurotransmitters [[serotonin]], [[noradrenaline]] (and [[adrenaline]]), and [[dopamine]]. However there are also a number of pharmaceuticals and research chemicals that act as reuptake inhibitors for other neurotransmitters such as [[glutamate]], [[GABA]], glycine, adenosine, choline (the precursor of [[acetylcholine]]), and the endocannabinoids, among others.
+Most known reuptake inhibitors affect the monoamine neurotransmitters [[serotonin]], [[noradrenaline]] (and [[adrenaline]]), and [[dopamine]]. However, there are also a number of pharmaceuticals and [[research chemicals]] that act as reuptake inhibitors for other neurotransmitters such as [[glutamate]], [[GABA]], glycine, adenosine, choline (the precursor of [[acetylcholine]]), and the endocannabinoids, among others.
 ==Mechanism of action==
-[[File:Reuptake inhibitor.png|350px|thumb|right|The effect of reuptake inhibitors on the presynaptic neurone.]]
+[[File:Reuptake inhibitor.png|350px|thumb|right|The effect of reuptake inhibitors on the presynaptic neurone]]
 Standard reuptake inhibitors are believed to act simply as competitive substrates that work by binding directly to the plasmalemma transporter of the [[neurotransmitter]] in question. They occupy the transporter in place of the respective neurotransmitter and competitively block the neurotransmitter from being transported from the synapse into the presynaptic neurone.
-Alternatively, some reuptake inhibitors bind to allosteric sites and inhibit reuptake indirectly and noncompetitively. Several dissociative drugs have been shown to work this way, including [[Phencyclidine|PCP]] and related drugs [[ketamine]], and dizocilpine (MK-801). They appear to exert their reuptake inhibition by binding to allosteric sites on each of the respective monoamine transporters. In addition to their high affinity for the main site of the monoamine transporters, several competitive transporter substrates, such as [[cocaine]], have lower affinity for these allosteric sites as well.
+Alternatively, some reuptake inhibitors bind to allosteric sites and inhibit reuptake indirectly and noncompetitively. Several [[dissociative]] drugs have been shown to work this way, including [[Phencyclidine|PCP]] and related drugs [[ketamine]], and [[dizocilpine]] (MK-801). They appear to exert their reuptake inhibition by binding to allosteric sites on each of the respective monoamine transporters. In addition to their high affinity for the main site of the monoamine transporters, several competitive transporter substrates, such as [[cocaine]], have lower affinity for these allosteric sites as well.
 ==Types of reuptake inhibitors==
-*A '''selective reuptake inhibitor''' will inhibit the reuptake of a specific [[neurotransmitter]]. An example of this is the class of antidepressants known as selective serotonin reuptake inhibitors, or SSRIs.
+*A '''selective reuptake inhibitor''' will inhibit the reuptake of a specific [[neurotransmitter]]. An example of this is the class of antidepressants known as selective serotonin reuptake inhibitors, or [[SSRIs]].
-*A '''non-selective reuptake inhibitor''' will inhibit the reuptake of more than one type of [[neurotransmitter]]. An example of this is [[cocaine]], which acts as a serotonin-noradrenaline-dopamine reuptake inhibitor, or SNDRI.
+*A '''non-selective reuptake inhibitor''' will inhibit the reuptake of more than one type of [[neurotransmitter]]. An example of this is [[cocaine]], which acts as a serotonin-noradrenaline-dopamine reuptake inhibitor, or [[SNDRI]].
 ==See also==